目的:测定穿心莲内酯和脱水穿心莲内酯在正辛醇-水和正辛醇-缓冲液体系中的表观油水分配系数,为体内吸收研究提供参考。方法:采用摇瓶法测定穿心莲内酯和脱水穿心莲内酯的表观油水分配系数,采用HPLC法测定穿心莲内酯和脱水穿心莲内酯的浓度。结果:37℃下穿心莲内酯和脱水穿心莲内酯表观油水分配系数分别为3.90(10gPapp=0.59)和19.75(10gPapp=1.30)。结论:pH对穿心莲内酯和脱水穿心莲内酯表观油水分配系数有一定影响。在一定范围内,pH值增加可使穿心莲内酯和脱水穿心莲的表观油水分配系数减小。穿心莲内酯在pH6的磷酸盐缓冲液时表观油水分配系数最大[2.62(10gPapp=0.42)],脱水穿心莲内酯则在pH5时达到最大[25.19(10gPapp=1.40)]。
Objective:To determine the apparent n-octanol-water/ buffer partition coefficient of andrographolide and dehydroan- drographolide. Methods : The apparent n-octanol-water/buffer partition coefficients of andrographolide and dehydroandrographolide were measured by shaking flask method. The concentrations of andrographolide and dehydroandrographolide were analyzed by HPLC method. Results : The Papp of andrographolide and dehydroandrographolide were 3.90 ( log Papp = 0. 59 ) and 19. 75 ( log Papp = 1.30) in water at 37℃, respectively. Conclusions:The apparent n-octanol-buffer partition coefficients of andrographolide and dehydroandrographolide are influenced by pH, and the higher pH may decrease the apparent n-octanol-buffer partition coefficients of them. Andrographolide has the highest partition coefficient in pH6, and dehydroandrogapholide in pH5.